Thalidomide and its derivatives lenalidomide and pomalidomide (IMiDs) are effective
treatments of haematologic malignancies. It was shown that IMiDs impart gain-of-function …

Inducing protein degradation via small molecules is a transformative therapeutic paradigm.
Although structural requirements of target degradation are emerging, mechanisms …

Cereblon (CRBN), originally identified as a gene associated with intellectual disability, was
identified as primary target of thalidomide. Accumulating evidence has shown that CRBN is …

Highlights•E3 ligases recruit substrates for proteasomal degradation by recognition of
degrons.•Crystal structures reveal the structural basis and mechanism of degron …

Recent evidence has revealed that senescence induction requires fine-tuned activation of
p53, however, mechanisms underlying the regulation of p53 activity during senescence …

In the last decade, the ubiquitin–proteasome system has emerged as a valid target for the
development of novel therapeutics. E3 ubiquitin ligases are particularly attractive targets …

The bromodomain‐containing proteins BRD9 and BRD7 are part of the human SWI/SNF
chromatin‐remodeling complexes BAF and PBAF. To date, no selective inhibitor for BRD7/9 …

Chemical biology strategies for directly perturbing protein homeostasis including the
degradation tag (dTAG) system provide temporal advantages over genetic approaches and …

SUMO-targeted ubiquitin ligases (STUbLs) mediate the ubiquitylation of SUMOylated
proteins to modulate their functions. In search of direct targets for the STUbL RNF4, we have …

Targeted protein degradation through chemical hijacking of E3 ubiquitin ligases is an
emerging concept in precision medicine. The ubiquitin code is a critical determinant of the …